Tiziano Tuccinardi
University of Pisa
Virtual screeningChemical synthesisSelectivityCancerDocking (molecular)Cannabinoid receptorQuantitative structure–activity relationshipReceptorMolecular modelEnzymeChemistryStructure–activity relationshipCarbonic anhydraseLactate dehydrogenaseEndocannabinoid systemCancer researchBiochemistryComputational biologyStereochemistryMonoacylglycerol lipaseBiologyCancer cellPharmacology
Publications 253
In silico target fishing, whose aim is to identify possible protein targets for a query molecule, is an emerging approach used in drug discovery due its wide variety of applications. This strategy allows the clarification of mechanism of action and biological activities of compounds whose target is still unknown. Moreover, target fishing can be employed for the identification of off targets of drug candidates, thus recognizing and preventing their possible adverse effects. For these reasons, tar...
#1Vibhu Jha (UniPi: University of Pisa)H-Index: 3
#2Salvatore Galati (UniPi: University of Pisa)H-Index: 2
Last. Tiziano Tuccinardi (UniPi: University of Pisa)H-Index: 35
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: ATP citrate lyase (ACLY) is an important enzyme that catalyzes the conversion of citrate to acetyl-CoA in normal cells, facilitating the de novo fatty acid synthesis. Lipids and fatty acids were found to be accumulated in different types of tumors, such as brain, breast, rectal and ovarian cancer, representing a great source of energy for cancer cell growth and metabolism. Since ACLY-mediated conversion of citrate to acetyl-CoA constitutes the basis for fatty acid synthesis, ACLY seems to be q...
#1Giulia Bononi (UniPi: University of Pisa)H-Index: 5
#2Tiziano Tuccinardi (UniPi: University of Pisa)H-Index: 35
Last. Carlotta Granchi (UniPi: University of Pisa)H-Index: 24
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Much of the experimental evidence in the literature has linked altered lipid metabolism to severe diseases such as cancer, obesity, cardiovascular pathologies, diabetes, and neurodegenerative diseases. Therefore, targeting key effectors of the dysregulated lipid metabolism may represent an effective strategy to counteract these pathological conditions. In this context, α/β-hydrolase domain (ABHD) enzymes represent an important and diversified family of proteins, which are involved in the complex...
#1Simona Mattioli (University of Perugia)H-Index: 15
#2Gisella Paci (UniPi: University of Pisa)H-Index: 14
Last. Simone Mancini (UniPi: University of Pisa)H-Index: 14
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Abstract The capability of some insects to be reared on by-products, waste and former foodstuff make them a very promising response to the increasing request of animals’ products. Mealworm larvae (Tenebrio molitor) are widely studied for feed and food purposes. In this study the effects of five diets were tested on the fatty acids (FA) profile, the lipid metabolism and the antioxidant molecules of the larvae. Three diets were composed by single ingredients as cookies, bread leftovers and brewery...
#1Giulia Bononi (UniPi: University of Pisa)H-Index: 5
#2Giacomo Tonarini (UniPi: University of Pisa)
Last. Carlotta Granchi (UniPi: University of Pisa)H-Index: 24
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Abstract null null Monoacylglycerol lipase (MAGL) is an enzyme belonging to the endocannabinoid system that mainly metabolizes the endocannabinoid 2-arachidonoylglycerol (2-AG). Numerous studies have shown the involvement of this enzyme in various pathological conditions such as pain, cancer progression, Parkinson's and Alzheimer's disease, thus encouraging the development of new MAGL modulators. In this context, we developed new diphenylsulfide-benzoylpiperidine derivatives characterized by a h...
The computer-aided drug design field is constituted by a wide range of different approaches that can be roughly classified as either ligand- or receptor-based techniques. In order to design and dev...
#1Shaohong Peng (CUHK: The Chinese University of Hong Kong)H-Index: 7
#2Pei Guo (SCUT: South China University of Technology)H-Index: 4
Last. Ho Yin Edwin ChanH-Index: 22
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DNA damage plays a central role in the cellular pathogenesis of polyglutamine (polyQ) diseases, including Huntington's disease (HD). In this study, we showed that the expression of untranslatable expanded CAG RNA per se induced the cellular DNA damage response pathway. By means of RNA sequencing (RNA-seq), we found that expression of the Nudix hydrolase 16 (NUDT16) gene was down-regulated in mutant CAG RNA-expressing cells. The loss of NUDT16 function results in a misincorporation of damaging nu...
1 CitationsSource
#2Giulio PoliH-Index: 17
Last. Isabella CaligiuriH-Index: 18
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Background The progression of ovarian cancer seems to be related to HDAC1, HDAC3 and HDAC6 activity. A possible strategy for improving therapies for treating ovarian carcinoma, minimizing the preclinical screenings, is the repurposing of already approved pharmaceutical products as inhibitors of these enzymes. Objective This work was aimed to implement a computational strategy for identifying new HDAC inhibitors for ovarian carcinoma treatment among approved drugs. Method The CHEMBL database was ...
#2Gloria SaorinH-Index: 2
Last. Flavio RizzolioH-Index: 28
view all 12 authors...